GPR39-C3, GPR39 Agonist


Catalog No. size PriceQuantity
M60209-2S 2 mg solid $144
M60209-10S 10mg solid $563

Description

GPR39-C3 is the first potent, selective and orally bioavailable GPR39 agonist with an EC50 ~0.8 nM for human GPR39 and ~0.4 nM for rodent GPR39. It has no inhibitory effects (at 10 μM) on a panel of kinases and exhibits no relevant binding affinity for the related ghrelin and neurotensin-1 receptors and other enzymes, transporters, and GPCRs. GPR39-C3 has excellent functional activity in physiologically relevant rodent cells and in vivo. An acute study in normal mice with orally administrated GPR39-C3 confirmed in vitro findings by demonstrating an increase of the relevant pharmacodynamic marker GLP-1. It is a good chemical tool to enable interrogation of GPR39 signaling in different cellular contexts.

Product information

CAS Number: 1621175-65-2

Molecular Weight: 418.90

Formula: C18H19ClN6O2S

Chemical Name: N-(3-chloro-4-(((2-(methylamino)-6-(pyridin-2-yl)pyrimidin-4-yl)amino)methyl)phenyl)methanesulfonamide

Smiles: CNC1=NC(=CC(NCC2=CC=C(C=C2Cl)NS(C)(=O)=O)=N1)C1=CC=CC=N1

InChiKey: DRSZMILOMUPIBJ-UHFFFAOYSA-N

InChi: InChI=1S/C18H19ClN6O2S/c1-20-18-23-16(15-5-3-4-8-21-15)10-17(24-18)22-11-12-6-7-13(9-14(12)19)25-28(2,26)27/h3-10,25H,11H2,1-2H3,(H2,20,22,23,24)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

GPR39-C3 was used at 0.1-1 µM final concentration in various in vitro assays.

In Vivo:

GPR39-C3 was dosed to Male C57BL/6 mice via oral gavage at 30 mg/kg, concurrently with DPP4 inhibitor PKF275-055 (3 mg/kg). The animals were challenged orally after 1 hour with a glucose bolus (3 g/kg) and active GLP-1 levels were measured 30 min later by MSD Active GLP-1 Assay kit. Formulation is 0.5% methylcellulose/0.1% Tween 80 in water.

References:

  1. Stefan Peukert, et al. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists. (2014) ACS Med. Chem. Lett. In press.
  2. Bassilana F, et al. Target identification for a Hedgehog pathway inhibitor reveals the receptor GPR39. (2014) Nat Chem Biol. 10(5):343-9.

Products are for research use only. Not for human use.

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